Arvinas Announces Pipeline Programs Targeting Validated and Classically “Undruggable” Disease-Causing Proteins
- Category: Small Molecules
- Published on Wednesday, 14 October 2020 18:57
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NEW HAVEN, CT, USA I October 14, 2020 I Arvinas, Inc. (Nasdaq: ARVN), a clinical-stage biotechnology company creating a new class of drugs based on targeted protein degradation, today announced platform updates and disclosed five additional programs from its preclinical pipeline. Arvinas’ portfolio encompasses a range of validated and undruggable targets in oncology, immuno-oncology, and neuroscience.
“We continue to expand our pipeline and further our leadership position in targeted protein degradation by leveraging the PROTAC® Discovery Engine, our integrated platform that we’ve been advancing since 2013,” said John Houston, Ph.D., President and Chief Executive Officer of Arvinas. “With the programs introduced today, and the important breakthroughs we’ve made over the years – such as achieving oral bioavailability in human patients and successfully penetrating the blood-brain barrier in preclinical studies – we make it clear that we have the ability to rapidly progress Arvinas’ deep pipeline in order to benefit patients in multiple areas of high unmet need.”
“The targets we announced today represent a mix of oncology, immuno-oncology and neuroscience programs,” said Ian Taylor, Ph.D., Chief Scientific Officer of Arvinas. “Our progress with classic ‘undruggable’ targets like KRAS reinforces our commitment to finding solutions for patients and demonstrates the power of Arvinas’ PROTAC® Discovery Engine in generating novel therapies.”
In addition to progressing its platform and preclinical pipeline, Arvinas is testing two PROTAC® protein degraders in human clinical trials: ARV-110 for the treatment of men with metastatic castrate-resistant prostate cancer and ARV-471 for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer. Arvinas plans to share updated data for these programs later in the fourth quarter of 2020.
Newly Announced Programs
- B-cell lymphoma 6 protein (BCL6) is a transcriptional repressor implicated in B cell lymphomas and facilitates B cell tolerance of rapid proliferation and somatic gene recombination via repressing cell cycle checkpoints, terminal differentiation, apoptosis, and the DNA damage response. PROTAC®-mediated degradation would address the scaffolding function of BCL6. Arvinas anticipates filing an IND for this program in 2022.
- Kirsten rat sarcoma (KRAS) is a classic “undruggable” target, due to its lack of deep “pockets,” and is associated with poor prognosis and resistance to standards of care in several tumor types. Arvinas is developing pan-KRAS mutant and mutant-specific KRAS degraders, e.g., G12D and G12V. Arvinas anticipates filing an IND for this program in 2023.
- Myelocytomatosis (Myc) proteins are implicated in up to 70% of all human cancers. Targeting Myc indirectly, such as by inhibiting transcription modulators, has not been successful, but PROTAC®-mediated degradation has the potential to directly target and degrade Myc. This is an Exploratory-stage program.
- Hematopoietic progenitor kinase 1 (HPK1) is a suppressor of T cell activation and targeting HPK1 can enhance anti-tumor immune responses. PROTAC®-mediated degradation has the potential to address the proposed scaffolding component of HPK1’s activity. This is an Exploratory-stage program.
- Huntington’s disease is caused by a mutation in the huntingtin (HTT) gene. PROTAC® degradation has the potential to allow the selective targeting of mutant HTT protein without impacting wild-type HTT protein. This is an Exploratory-stage program.
Arvinas is a clinical-stage biopharmaceutical company dedicated to improving the lives of patients suffering from debilitating and life-threatening diseases through the discovery, development, and commercialization of therapies that degrade disease-causing proteins. Arvinas uses its proprietary PROTAC® Discovery Engine platform to engineer proteolysis targeting chimeras, or PROTAC® targeted protein degraders, that are designed to harness the body’s own natural protein disposal system to selectively and efficiently degrade and remove disease-causing proteins. In addition to its robust preclinical pipeline of PROTAC® protein degraders against validated and “undruggable” targets, the company has two clinical-stage programs: ARV-110 for the treatment of men with metastatic castrate-resistant prostate cancer; and ARV-471 for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer. For more information, visit www.arvinas.com.